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Updated: May 24, 2025

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
Tasurgratinib Succinate: First Approval
1Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand. dru@adis.com.
Abstract:
Tasurgratinib succinate (TASFYGO®; Eisai Co., Ltd.) is an orally active, small molecule inhibitor of fibroblast growth factor receptors (FGFRs) 1, 2, and 3 being developed for the treatment of solid tumors, including cholangiocarcinoma (i.e., bile duct cancer) and breast cancer. Tasurgratinib succinate received its first approval on 24 September 2024 in Japan, for the treatment of FGFR2 fusion-positive unresectable biliary tract cancer that has progressed after chemotherapy. The approval was based on the positive results of an open-label, single-arm, multicenter, phase II study conducted in Japan and China. This article summarizes the milestones in the development of tasurgratinib succinate leading to this first approval for biliary tract cancer.
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